Terfenadine

Terfenadine ((±) -Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM[1]. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9[2].

Product Specifications

CAS Number

[50679-08-8]

Product Name Alternative

(±) -Terfenadine; MDL-991

UNSPSC

12352005

Hazard Statement

H413

Target

Apoptosis; Caspase; Histamine Receptor; Na+/Ca2+ Exchanger; Potassium Channel

Type

Reference compound

Related Pathways

Apoptosis; GPCR/G Protein; Immunology/Inflammation; Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Cancer-programmed cell death

Field of Research

Cancer; Inflammation/Immunology; Endocrinology

Assay Protocol

https://www.medchemexpress.com/Terfenadine.html

Concentration

10mM

Purity

99.98

Solubility

DMSO : ≥ 50 mg/mL|H2O : < 0.1 mg/mL

Smiles

OC(C1=CC=C(C(C)(C)C)C=C1)CCCN2CCC(C(C3=CC=CC=C3)(O)C4=CC=CC=C4)CC2

Molecular Formula

C32H41NO2

Molecular Weight

471.67

Precautions

H413

References & Citations

[1]Kamiya K, et al. Molecular determinants of hERG channel block by terfenadine and cisapride. J Pharmacol Sci. 2008 Nov;108 (3) :301-307.|[2]Nicolau-Galmés F, et al. Terfenadine induces apoptosis and autophagy in melanoma cells through ROS-dependent and -independent mechanisms. Apoptosis. 2011 Dec;16 (12) :1253-67.|[3]An L, et al. Terfenadine combined with epirubicin impedes the chemo-resistant human non-small cell lung cancer both in vitro and in vivo through EMT and Notch reversal. Pharmacol Res. 2017 Oct;124:105-115.